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  ONCOgenic GPCR Network of Excellence and Training



Publications ONCORNET:


From insight to modulation of CXCR4 and ACKR3 (CXCR7) function

Smit MJ, van Muilwijk-Koezen JE.

Mol Pharmacol. 2019 Oct 17. pii: mol.119.118364. doi: 10.1124/mol.119.118364 [Epub ahead of print]

PMID: 31624136


Modulators of CXCR4 and CXCR7/ACKR3 function

Adlere I, Caspar B, Arimont M, Dekkers S, Visser K, Stuijt J, de Graaf C, Stocks M, Kellam B, Briddon S, Wijtmans M, de Esch I, Hill S, Leurs R.

Mol Pharmacol. 2019 Sep 23. pii: mol.119.117663. doi: 10.1124/mol.119.117663 [Epub ahead of print]

PMID: 31548340


Antibodies targeting chemokine receptors CXCR4 and ACKR3

Bobkov V, Arimont M, Zarca A, De Groof T, van der Woning B, de Haard H, Smit MJ.

Mol Pharmacol. 2019 Sep 3. pii: mol.119.116954. doi: 10.1124/mol.119.116954 [Epub ahead of print]

PMID: 31481460


Chemokine receptor crystal structures: what can be learnt from them?

Arimont M, Hoffmann C, de Graaf C, Leurs R.

Mol Pharmacol. 2019 Jul 2. pii: mol.119.117168. doi: 10.1124/mol.119.117168 [Epub ahead of print]

PMID: 31266800


Context-dependent signalling of CXC chemokine receptor 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3)

Heuninck J, Perpina Viciano C, Işbilir A, Caspar B, Capoferri D, Briddon SJ, Durroux T, Hill SJ, Lohse MJ, Milligan G, Pin JP, Hoffmann C.

Mol Pharmacol. 2019 May 15. pii: mol.118.115477. doi:10.1124/mol.118.115477 [Epub ahead of print]

PMID: 31092552


Atypical chemokine receptor 3 (ACKR3): a comprehensive overview of its expression and potential roles in the immune system

Koenen J, Bachelerie F, Balabanian K, Schlecht-Louf G, Gallego C.  



Time-Resolved FRET-Based Assays to Characterize G Protein-Coupled Receptor Hetero-oligomer Pharmacology

Heuninck J, Hounsou C, Dupuis E, Trinquet E, Mouillac B, Pin JP, Bonnet D, Durroux T.

Methods Mol Biol. 2019;1947:151-168. doi:10.1007/978-1-4939-9121-1_8





Nanobodies: New avenues for imaging, stabilizing and modulating GPCRs

De Groof TWM, Bobkov V, Heukers R, Smit MJ.

Mol Cell Endocrinol. 2019 March 15;484: 15-24. DOI: 10.1016/j.mce.2019.01.021 Epub 2019 Jan 26



CXCR4/ACKR3 phosphorylation and recruitment of interacting proteins: key mechanisms regulating their functional status

Fumagalli A, Zarca A, Neves M, Casper B, Hill S, Mayor F Jr., Smit MJ, Marin P.

Mol Pharmacol. 2019 March 5 [Epub ahead of print], mol.118.115360,




The role of ACKR3 in breast, lung and brain cancer

Neves M, Fumagalli A, van den Bor J, Marin P, Smit MJ, Mayor F Jr.

Mol Pharmacol. 2019 Feb 11 (Epub ahead of print). DOI: 10.1124/mol.118.115279



Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists

Adlere I, Sun S, Zarca A, Roumen L, Gozelle M, Viciano CP, Caspar B, Arimont M, Bebelman JP, Briddon SJ, Hoffmann C, Hill SJ, Smit MJ, Vischer HF, Wijtmans M, de Graaf C, de Esch IJP, Leurs R.

Eur J Med Chem. 2019 Jan 15;162:631-649. DOI: 10.1016/j.ejmech.2018.10.060 Epub 2018 Oct 30



CXCR4-targeting nanobodies differentially inhibit CXCR4 function and HIV entry

Van Hout A, Klarenbeek A, Bobkov V, Doijen J, Arimont M, Zhao C, Heukers R, Rimkunas R, de Graaf C, Verrips T, van der Woning B, de Haard H, Rucker JB, Vermeire K, Handel T, Van Loy T, Smit MJ, Schols D.

Biochem Pharmacol. 2018 Dec;158:402-412. DOI: 10.1016/j.bcp.2018.10.015 Epub 2018 Oct 17



Nanobody-Fc constructs targeting chemokine receptor CXCR4 potently inhibit signaling and CXCR4-mediated HIV-entry and induce antibody effector functions

Bobkov V, Zarca AM, Van Hout A, Arimont M, Doijen J, Bialkowska M, Toffoli E, Klarenbeek A, van der Woning B, van der Vliet HJ, Van Loy T, de Haard H, Schols D, Heukers R, Smit MJ.

Biochem Pharmacol. 2018 Dec;158:413-424. DOI: 10.1016/j.bcp.2018.10.014 Epub 2018 Oct 17



G protein-coupled receptor kinases (GRKs) in tumorigenesis and cancer progression: GPCR regulators and signaling hubs

Nogués L, Palacios-García J, Reglero C, Rivas V, Neves M, Ribas C, Penela P, Mayor F Jr. Semin Cancer Biol 2018 Feb;48:78-90. DOI: 10.1016/j.semcancer.2017.04.013 Epub 2017 May 1



Structural Analysis of Chemokine Receptor-Ligand Interactions

Arimont M, Sun SL, Leurs R, Smit M, de Esch IJP, de Graaf C.

J Med Chem. 2017 Jun 22;60(12):4735-4779. doi: 10.1021/acs.jmedchem.6b01309 Epub 2017 Mar 10



G-Protein-Coupled Receptor Kinase 2 as a Potential Modulator of the Hallmarks of Cancer

Nogués L, Reglero C, Rivas V, Neves M, Penela P, Mayor F Jr.

Mol Pharmacol. 2017 Mar;91(3):220-228. doi: 10.1124/mol.116.107185 Epub 2016 Nov 28



Fluorescent-Based Strategies to Investigate G Protein-Coupled Receptors: Evolution of the Techniques to a Better Understanding

Faklaris O, Heuninck J, Falco A, Goyet E, Zwier JM, Pin JP, Mouillac B, Perroy J, Durroux T.

Topics in Medicinal Chemistry, chapter May 2017 DOI: 10.1007/7355_2017_2



Peripheral Interaction of Resolvin D1 and E1 with Opioid Receptor Antagonists for Antinociception in Inflammatory Pain in Rats

Oehler B, Mohammadi M, Perpiñá Viciano C, Hackel D, Hoffmann C, Brack A, Rittner HL.

Front Mol Neurosci. 2017 Aug 3;10:242. DOI: 10.3389/fnmol.2017.00242 eCollection 2017



CXCR4-Specific Nanobodies as Potential Therapeutics for WHIM syndrome

de Wit RH, Heukers R, Brink HJ, Arsova A, Maussang D, Cutolo P, Strubbe B, Vischer HF, Bachelerie F, Smit MJ.

J Pharmacol Exp Ther. 2017 Oct;363(1):35-44. DOI: 10.1124/jpet.117.242735 Epub 2017 Aug 2



DNA immunization combined with scFv phage display identifies antagonistic GCGR specific antibodies and reveals new epitopes on the small extracellular loops

van der Woning B, De Boeck G, Blanchetot C, Bobkov V, Klarenbeek A, Saunders M, Waelbroeck M, Laeremans T, Steyaert J, Hultberg A, De Haard H.

MAbs. 2016 Aug-Sep;8(6):1126-35. doi: 10.1080/19420862.2016.1189050 Epub 2016 May 21



G protein-coupled receptor kinase 2 (GRK2) promotes breast tumorigenesis through a novel HDAC6-Pin1 axis

Nogués L, Reglero C, Rivas V, Salcedo A, Lafarga V2, Neves M, Ramos P, Mendiola M, Berjón A, Stamatakis K, Zhou XZ, Lu KP, Hardisson D, Mayor F Jr, Penela P.

EBioMedicine. 2016 Nov;13:132-145. DOI: 10.1016/j.ebiom.2016.09.030 Epub 2016 Oct 1









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VU University Amsterdam
The Netherlands

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